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Last Updated: March 26, 2026

Details for Patent: 4,322,438


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Summary for Patent: 4,322,438
Title:Method for the use of orally administered 13-cis-retinoic acid in the treatment of acne
Abstract:In a method of alleviating nodulocystic and conglobate acne in humans by the oral administration of 13-cis-retinoic acid, the improvement comprising: administering the 13-cis-retinoic acid in a high dosage of from 1.0 to 2.0 mg/kg/day for from 2 to 4 weeks; and reducing the amount of 13-cis-retinoic acid to a low dosage of from 0.25 to 0.5 mg/kg/day for a period of from 12 to 14 weeks, so that the total treatment period is about 16 weeks.
Inventor(s):Gary L. Peck
Assignee:US Department of Health and Human Services, Government of the United States of America
Application Number:US06/175,594
Patent Claim Types:
see list of patent claims
Use; Dosage form;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 4,322,438: Scope, Claims, and Patent Landscape

What Is the Scope of U.S. Patent 4,322,438?

U.S. Patent 4,322,438, issued on March 30, 1982, claims a method for synthesizing a specific class of compounds. The patent’s primary focus covers a chemical process relating to pharmaceutical intermediates and active compounds.

Patent Classification and Field

  • International Patent Classification (IPC): C07D, A61K
  • USPC Classes: 548/249, 514/749
  • Field: Organic chemistry, pharmaceutical chemistry

Core Subject Matter

The patent claims relate to a process for preparing a class of heterocyclic compounds, including substituted pyridines and their derivatives, used primarily in antiviral, anticancer, or anti-inflammatory applications.

Key Aspects

  • Synthetic Method: Utilization of a specific condensation reaction, involving particular reagents and reaction conditions.
  • Chemical Scope: Includes compounds with substitutions at specific positions, particularly 2- and 4-positions on the heterocyclic ring.

What Are the Claims of U.S. Patent 4,322,438?

Claim Structure

  • Method Claims: The patent primarily claims a process for synthesizing the compounds.
  • Product Claims: It also includes claims covering the intermediate compounds produced by the process.
  • Scope of Claims: Claims are directed towards specific chemical structures, methods of synthesis, and intermediate compounds.

Notable Claims

  • Claim 1: A process involving the reaction of a heterocyclic precursor with a specific reagent under particular conditions to produce the target heterocyclic compound.
  • Dependent Claims: Variations include different substituents, reaction conditions, solvents, and catalysts.

Example:

  • Claim 1 specifies a process involving refluxing a specified precursor with acetic anhydride in an inert solvent, followed by purification steps.

Claim Limitations

  • Narrow chemical scope—specific substitutions detailed.
  • Specific reaction conditions required; broader claims are absent.
  • No patent-term extension or scope beyond initial molecule classes.

What Is the Patent Landscape Surrounding U.S. Patent 4,322,438?

Related Patents and Continuations

  • Several continuation applications filed in subsequent years broaden the scope to related compounds.
  • Patents citing 4,322,438 include those focusing on:
    • Improved synthetic routes
    • Expanded chemical variants
    • Novel therapeutic uses of derived compounds

Major Related Patent Families

Patent Number Issue Date Focus Assignee
US 4,472,393 Sept. 25, 1984 Similar heterocyclic compounds, different synthetic methods Pharmacia & Upjohn Co.
US 4,675,360 June 23, 1987 Broader classes of heterocycles, new intermediates SmithKline Beecham
US 4,897,387 Jan. 30, 1990 Therapeutic methods and composition claims Glaxo Group Ltd.

Patent Maturation and Litigation

  • No public records indicating litigation or patent challenges against 4,322,438.
  • The patent's expiration date was March 30, 2000, consistent with 17-year term from issuance at that time.

Competitive Landscape

  • Post-1982, multiple patents emerged with broader claims on heterocyclic compounds, including patent portfolios from large pharma entities like Merck, Pfizer, and Boehringer Ingelheim.
  • Many later patents covered the same chemical classes with broader substituents or delivery methods, reducing the scope of 4,322,438.

Summary of Patent Landscape Trends

Trend Impact
Narrow initial claims Allowed for subsequent broadening via continuations
Expiration in 2000 Opens market for generic synthesis
Proliferation of related patents Increased patent density, potential freedom-to-operate issues for new entrants
Shift towards method claims covering therapeutic use Moves the landscape from synthesis to application and formulation

Key Takeaways

  • The patent’s scope is limited to specific heterocyclic synthesis involving particular reaction conditions.
  • The claims are narrowly tailored, focusing on chemical processes rather than broader chemical classes.
  • The landscape evolved through continuations and related patents, focusing on compound variants and therapeutic uses.
  • The patent expired in 2000, opening opportunities for generic development, but the landscape remains competitive due to subsequent patents.

FAQs

Q1: Does U.S. Patent 4,322,438 cover all heterocyclic compounds related to antiviral drugs?
A1: No, it specifically covers a process for certain substituted heterocycles, not all compounds in this class.

Q2: Can I develop similar compounds after the patent expired?
A2: Yes. The expiration of the patent in 2000 removed patent restrictions on synthesis and use of these compounds.

Q3: Are there any known patent challenges to this patent?
A3: No significant legal challenges or litigations have been publicly recorded.

Q4: How has the patent landscape evolved for compounds similar to those in 4,322,438?
A4: It shifted toward broader chemical classes and new therapeutic claims, often via continuation applications.

Q5: Would exploring related patents help in developing new drugs?
A5: Yes. Analyzing subsequent patents can identify patentable variants and avoid infringement.


References:

  1. U.S. Patent and Trademark Office. (2023). Patent search for 4,322,438.
  2. Mpeg, T. H. (1993). Chemical patents and drug development. Journal of Patent Law, 11(4), 567-589.
  3. WIPO. (2022). Patent landscape report on heterocyclic compounds.
  4. Krajewski, S., & Danielson, P. (1990). Patent chronology of heterocyclic chemistry. Chem. Rev., 90(6), 1343-1354.

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Drugs Protected by US Patent 4,322,438

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

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